Identification of a diverse synthetic abietane diterpenoid library and insight into the structure-activity relationships for antibacterial activity. Issue 24 (15th December 2017)

• Record Type: Journal Article
• Authors: Hou, Wei; Zhang, Guanjun; Luo, Zhi; Li, Di; Ruan, Haoqiang; Ruan, Benfang Helen; Su, Lin; Xu, Hongtao
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 27:Issue 24(2017)
• Page Start: 5382
• Page End: 5386
• Publication Date: 2017-12-15
• Subjects: Diterpenoid -- Natural product-like (NPL) -- Dehydroabietic acid (DHAA) -- Abietic acid (AA) -- Click chemistry -- Antibacterial; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2017.11.014
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: A diverse natural product-like (NPL) synthetic abietane diterpenoid library containing 86 compounds were obtained and the SARs were studied based on their antibacterial potential. Further in vitro cytotoxic and in silico drug-like properties evaluation showed that the potent antibacterial compound84 had good drug-like properties and displayed low cytotoxicity toward noncancerous mammalian cells, indicating the study of AA and DHAA might be a good starting point for the search of novel antimicrobial molecules. Future work should be focused on the optimization of their potency and selectivity.